Ontology highlight
ABSTRACT:
SUBMITTER: Thorsell AG
PROVIDER: S-EPMC5934274 | biostudies-literature | 2017 Feb
REPOSITORIES: biostudies-literature
Thorsell Ann-Gerd AG Ekblad Torun T Karlberg Tobias T Löw Mirjam M Pinto Ana Filipa AF Trésaugues Lionel L Moche Martin M Cohen Michael S MS Schüler Herwig H
Journal of medicinal chemistry 20161221 4
Selective inhibitors could help unveil the mechanisms by which inhibition of poly(ADP-ribose) polymerases (PARPs) elicits clinical benefits in cancer therapy. We profiled 10 clinical PARP inhibitors and commonly used research tools for their inhibition of multiple PARP enzymes. We also determined crystal structures of these compounds bound to PARP1 or PARP2. Veliparib and niraparib are selective inhibitors of PARP1 and PARP2; olaparib, rucaparib, and talazoparib are more potent inhibitors of PAR ...[more]